1. Membrane Transporter/Ion Channel
  2. Na+/Ca2+ Exchanger Sodium Channel
  3. Benzamil hydrochloride

Benzamil hydrochloride  (Synonyms: Benzylamiloride hydrochloride)

Cat. No.: HY-B1546A Purity: 99.80%
SDS COA Handling Instructions

Benzamil hydrochloride (Benzylamiloride hydrochloride), an Amiloride analogue, is a Na+/Ca2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil hydrochloride also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil hydrochloride inhibits TRPP3-mediated Ca2+-activated currents, with an IC50 of 1.1 μM.

For research use only. We do not sell to patients.

Benzamil hydrochloride Chemical Structure

Benzamil hydrochloride Chemical Structure

CAS No. : 161804-20-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
5 mg USD 60 In-stock
10 mg USD 79 In-stock
50 mg USD 260 In-stock
100 mg USD 460 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Benzamil hydrochloride (Benzylamiloride hydrochloride), an Amiloride analogue, is a Na+/Ca2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil hydrochloride also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil hydrochloride inhibits TRPP3-mediated Ca2+-activated currents, with an IC50 of 1.1 μM[1][2][3].

In Vitro

Benzamil hydrochloride (Benzylamiloride hydrochloride) inhibits neuronal and heterologously expressed small conductance Ca2+-activated K2+ channels[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Benzamil hydrochloride (Benzylamiloride hydrochloride) (0.7 mg/kg/day; s.c.) treated stroke-prone spontaneously hypertensive rats (SHRSP) survived, on average, until 16.1 weeks of age in SHRSP rats[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

356.21

Formula

C13H15Cl2N7O

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=NC(Cl)=C(N)N=C1N)NC(NCC2=CC=CC=C2)=N.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (280.73 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8073 mL 14.0367 mL 28.0733 mL
5 mM 0.5615 mL 2.8073 mL 5.6147 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.02 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.02 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.80%

References
Cell Assay
[2]

Individual CCD segments are dissected from rabbit and mouse kidney.The measurements of [Na+]i are used as a reflection of Na+ transport across the apical membrane. EnaC-specific activity is assessed by applying 10−6 M of the ENaC blocker Benzamil hydrochloride, a concentration that does not affect Na+:H+ exchange. Experiments are performed in the presence/absence of luminal Benzamil hydrochloride or the Na:H exchanger blocker HOE694 administers with/without the AT1 receptor blocker candesartan. Final DMSO concentrations are below 0.1% [2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

For the acute intracerebroventricular injection in anesthetized rats. A guide cannula is inserted into the right lateral cerebral ventricle, and Benzamil hydrochloride (0.1 nmol/kg, n=6; 1 nmol/kg, n=6; 10 nmol/kg,n=7) or vehicle (n=6) is injected into the right lateral ventricle through a cannula connected to a microsyringe 15 min before the start of intracerebroventricular infusion of hypertonic NaCl. Each injection consists of a volume of 10 μL deliver manually over a period of 30 s. To investigate the effects of Benzamil hydrochloride on the pressor response induced by intracerebroventricular injection of the pressor agent other than hypertonic NaCl, endothelin-1, which has a potent pressor action in the brain of rats, is intracerebroventricularly injected (1 nmol/10 μL) 15 min after the intracerebroventricular preinjection of Benzamil hydrochloride (10 nmol/kg, n=6) or the vehicle (n=6), and mean arterial pressure, heart rate, and abdominal sympathetic nerve firings are recorded for 20 min. Catheters are implanted into both the femoral artery and vein of 12-wk-old male rats anesthetized with urethan. Both catheters are filled with heparinized saline (50 U/mL). Fifteen minutes before the start of intracerebroventricular infusion of hypertonic NaCl, Benzamil hydrochloride (10 nmol/kg, n=6) or vehicle (10 μL, n=6) is injected into a tube connects to the femoral venous catheter by directly inserting the microsyringe, and 0.1 ml of isotonic saline solution is injected through the catheter to deliver the contents into the venous circulation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8073 mL 14.0367 mL 28.0733 mL 70.1833 mL
5 mM 0.5615 mL 2.8073 mL 5.6147 mL 14.0367 mL
10 mM 0.2807 mL 1.4037 mL 2.8073 mL 7.0183 mL
15 mM 0.1872 mL 0.9358 mL 1.8716 mL 4.6789 mL
20 mM 0.1404 mL 0.7018 mL 1.4037 mL 3.5092 mL
25 mM 0.1123 mL 0.5615 mL 1.1229 mL 2.8073 mL
30 mM 0.0936 mL 0.4679 mL 0.9358 mL 2.3394 mL
40 mM 0.0702 mL 0.3509 mL 0.7018 mL 1.7546 mL
50 mM 0.0561 mL 0.2807 mL 0.5615 mL 1.4037 mL
60 mM 0.0468 mL 0.2339 mL 0.4679 mL 1.1697 mL
80 mM 0.0351 mL 0.1755 mL 0.3509 mL 0.8773 mL
100 mM 0.0281 mL 0.1404 mL 0.2807 mL 0.7018 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Benzamil hydrochloride
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